In efforts to develop new treatments for brain cancer, scientists from Johns Hopkins Drug Discovery and the Kimmel Cancer Center’s Bloomberg~Kimmel Institute for Cancer Immunotherapy report they have altered the structure of an experimental drug that seems to enhance its ability to slip through the mostly impermeable blood-brain barrier. Results of their proof-of-concept experiments in monkeys, published Aug. 25 in the Journal of Medicinal Chemistry, show a tenfold better delivery of the drug to the brain compared with the rest of animals’ bodies.
The scientists began with an experimental anti-cancer drug cultivated from bacteria found in Peruvian soil more than 70 years ago. Called 6-diazo-5-oxo-L-norleucine, or DON, the drug blocks the cellular use of the protein building block glutamine. On its own, DON has shrunk tumors in clinical trials of people with a variety of advanced cancers, but its damage to the gastrointestinal system, a glutton for glutamine, ultimately proved too toxic for humans, say the scientists.
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